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Temanogrel

Name: Temanogrel
Brand: TargetMol
SKU: T17033
Price: 44 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T17033Cas No. 887936-68-7

Alias APD791

Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Temanogrel

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Purity: 99.24%

Catalog No. T17033Alias APD791Cas No. 887936-68-7

Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Pack Size	Price	Availability
1 mg	$44	In Stock
5 mg	$111	In Stock
10 mg	$165	In Stock
25 mg	$277	In Stock
50 mg	$393	In Stock
100 mg	$533	In Stock
200 mg	$691	In Stock
1 mL x 10 mM (in DMSO)	$121	In Stock

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Purity:99.24%

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
Targets&IC50	5-HT2A:4.9 nM (ki)
In vitro	Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis (IC50: 13±7 nM) [1][3].
In vivo	Plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6, and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h, and 2.25 h after the start of treatment in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment [3].
Synonyms	APD791

Chemical Properties

Molecular Weight	436.5
Formula	C₂₄H₂₈N₄O₄
Cas No.	887936-68-7
Smiles	COc1cccc(c1)C(=O)Nc1ccc(OCCN2CCOCC2)c(c1)-c1ccnn1C
Relative Density.	1.24 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (286.37 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2910 mL	11.4548 mL	22.9095 mL	114.5475 mL
5 mM	0.4582 mL	2.2910 mL	4.5819 mL	22.9095 mL
10 mM	0.2291 mL	1.1455 mL	2.2910 mL	11.4548 mL
20 mM	0.1145 mL	0.5727 mL	1.1455 mL	5.7274 mL
50 mM	0.0458 mL	0.2291 mL	0.4582 mL	2.2910 mL
100 mM	0.0229 mL	0.1145 mL	0.2291 mL	1.1455 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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